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Three new proline-rich cyclic nonapeptides, cycloleonuripeptides A: cyclo (-Gly-Pro-Pro-Pro-Tyr-Pro-Pro-Met-Ile-), B: cyclo (-Gly-Pro-Pro-Pro-Tyr-Pro-Pro-Met(O)-Ile-), and C: cyclo (-Gly-Pro-Pro-Pro-Tyr-Pro-Pro-Met(O)-Ile-), have been isolated from the fruits of Leonurus heterophyllus and their...
A mixture of phages displaying the wild type and four mutant Rtem β-lactamases was submitted to three rounds of selection by incubation with a biotinylated suicide inhibitor followed by chromatography on streptavidin coated beads. The final mixture of selected phages was shown to be made up of...
Several 2,3-diarylbenzopyrans have been evaluated in an ovariectomized rat model and found to exhibit tissue selective estrogen agonist activity on bone and serum lipid parameters. A structural model that accounts for the pharmacological similarity of these benzopyrans and the benzothiophene...
Further development of N -carboxyalkyl dipeptide inhibitors of stromelysin-1 (MMP-3) led to the discovery of C -carboxyalkyl dipeptide analogs with improved oral bioavailability. An in vivo assay of human MMP-3 mediated degradation of a macromolecular substrate in an extravascular space is...
A novel bifurcated nucleoside that bears an adenine group trimethylene linked to the 5-position of uracil, 5-(omega-adenylpropyl)-2′-deoxyuridine, has been synthesized and incorporated into a DNA dodecamer. This nucleoside is designed to both intercalate and hydrogen bond when incorporated into...
Simple bisubstrate analogs, Ad-El-Gn, Ad-E2-Gn, and Ad-E3-Gn, are designed to be proto-type adenine-arginine mimetic structures. Both Ad-El-Gn and Ad-E2-Gn inhibit PKA with IC 50 values similar to that of adenosine at 100 μM ATP and are more potent inhibitors than adenosine at physiologically...
Novel water-soluble camptothecin analogues with excellent antitumor activity have been designed and synthesized by total synthesis. The analogues were evaluated for cytotoxic activity against five tumor cell lines. The most potent analogue 6c exhibited significant antitumor activity at wider...
A previously described cembranolide diterpene from Lobophytum cristagalli was identified as a potent (IC 50 0.15 μM) inhibitor of farnesyl protein transferase (FPT). The compound showed selectivity for FPT as compared to the closely related enzyme geranylgeranyl protein transferase-1 (IC 50 5.3...
The 2 R and 2 S - endo isomers of N 6 -(5,6-epoxynorborn-2-yl)adenosine have been synthesised and shown to be potent agonists for the A 1 adenosine receptor. The 2 S - endo isomer was equipotent to N 6 -cyclopentyladenosine and 10- to 12-fold more potent than the 2 R - endo isomer.
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